Download MendeleySynthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1)
Miyashiro, J., Woods, K.W., Park, C.H., Liu, X., Shi, Y., Johnson, E.F., Bouska, J.J., Olson, A.M., Luo, Y., Fry, E.H., Giranda, V.L., Penning, T.D.(2009) Bioorg Med Chem Lett 19: 4050-4054
- PubMed: 19553114
- DOI: https://doi.org/10.1016/j.bmcl.2009.06.016
- Primary Citation of Related Structures:
3GJW - PubMed Abstract:
Based on screening hit 1, a series of tricyclic quinoxalinones have been designed and evaluated for inhibition of PARP-1. Substitutions at the 7- and 8-positions of the quinoxalinone ring led to a number of compounds with good enzymatic and cellular potency. The tricyclic quinoxalinone class is sensitive to modifications of both the amine substituent and the tricyclic core. The synthesis and structure-activity relationship studies are presented.
Organizational Affiliation:
Cancer Research, GPRD, Abbott Laboratories, 100 Abbott Park Rd., Abbott Park, IL 60064, USA. [email protected]
